EP3247399A4 - Crystalline forms of efinaconazole - Google Patents

Crystalline forms of efinaconazole Download PDF

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Publication number
EP3247399A4
EP3247399A4 EP15878656.6A EP15878656A EP3247399A4 EP 3247399 A4 EP3247399 A4 EP 3247399A4 EP 15878656 A EP15878656 A EP 15878656A EP 3247399 A4 EP3247399 A4 EP 3247399A4
Authority
EP
European Patent Office
Prior art keywords
efinaconazole
crystalline forms
crystalline
forms
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP15878656.6A
Other languages
German (de)
French (fr)
Other versions
EP3247399A1 (en
Inventor
Itai Adin
Hila ELAZARI-SHALOM
Ori RORILK
Yana Sery
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Wavelength Enterprises Ltd
Original Assignee
Wavelength Enterprises Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Wavelength Enterprises Ltd filed Critical Wavelength Enterprises Ltd
Publication of EP3247399A1 publication Critical patent/EP3247399A1/en
Publication of EP3247399A4 publication Critical patent/EP3247399A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
EP15878656.6A 2015-01-20 2015-12-02 Crystalline forms of efinaconazole Withdrawn EP3247399A4 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562105390P 2015-01-20 2015-01-20
PCT/IL2015/051171 WO2016116919A1 (en) 2015-01-20 2015-12-02 Crystalline forms of efinaconazole

Publications (2)

Publication Number Publication Date
EP3247399A1 EP3247399A1 (en) 2017-11-29
EP3247399A4 true EP3247399A4 (en) 2018-09-05

Family

ID=56416514

Family Applications (1)

Application Number Title Priority Date Filing Date
EP15878656.6A Withdrawn EP3247399A4 (en) 2015-01-20 2015-12-02 Crystalline forms of efinaconazole

Country Status (8)

Country Link
US (1) US20180002310A1 (en)
EP (1) EP3247399A4 (en)
JP (1) JP2018502165A (en)
CN (1) CN107427585A (en)
AU (1) AU2015379251A1 (en)
CA (1) CA2974180A1 (en)
IL (1) IL253479A0 (en)
WO (1) WO2016116919A1 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106995434A (en) * 2016-01-25 2017-08-01 广东东阳光药业有限公司 A kind of crystal formation of triazole antifungal agent and preparation method thereof
CN110770220B (en) * 2017-05-19 2022-08-12 科研制药株式会社 Preparation and purification method of efinaconazole
CA3115742C (en) * 2018-12-29 2023-10-03 Viwit Pharmaceutical Co., Ltd. Preparation method for efinaconazole
JP2021054781A (en) * 2019-09-26 2021-04-08 デボン エルエス，リミテッド Co-crystalline efinaconazole and method for producing the same

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2612859A1 (en) * 2010-08-31 2013-07-10 Kaken Pharmaceutical Co., Ltd. Method for producing 1-triazole-2-butanol derivative
WO2016181306A1 (en) * 2015-05-12 2016-11-17 Lupin Limited Process for the preparation of efinaconazole
WO2016193917A1 (en) * 2015-06-04 2016-12-08 Glenmark Pharmaceuticals Limited Process for the preparation of efinaconazole

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3437695B2 (en) * 1993-05-10 2003-08-18 科研製薬株式会社 Azolylamine derivative
DK0698606T3 (en) * 1993-05-10 1998-08-24 Kaken Pharma Co Ltd Azolylamine derivatives
WO2001007643A1 (en) * 1999-07-28 2001-02-01 Kaken Pharmaceutical Co., Ltd. Method for detecting pathogenic microorganism and antimicrobial agent, method for evaluating the drug effect of antimicrobial agent, and antimicrobial agents
DE602007009574D1 (en) * 2006-12-28 2010-11-11 Kaken Pharma Co Ltd Gel composition for the treatment of mycosis
WO2008124131A1 (en) * 2007-04-05 2008-10-16 The John Hopkins University Antifungal agents as neuroprotectants
US20090175810A1 (en) * 2008-01-03 2009-07-09 Gareth Winckle Compositions and methods for treating diseases of the nail
FR2938066B1 (en) * 2008-11-06 2010-12-17 Centre Nat Rech Scient SYSTEM AND METHOD FOR QUANTITATIVE ANALYSIS OF THE ELEMENTARY COMPOSITION OF LASER-INDUCED PLASMA SPECTROSCOPY MATERIAL (LIBS)
CN104292214B (en) * 2014-09-24 2017-04-05 南京华威医药科技开发有限公司 The synthetic method of Chinese mugwort Fluconazole and its intermediate
CN104327047B (en) * 2014-10-17 2016-04-06 苏州明锐医药科技有限公司 The preparation method of Ai Feikang azoles

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2612859A1 (en) * 2010-08-31 2013-07-10 Kaken Pharmaceutical Co., Ltd. Method for producing 1-triazole-2-butanol derivative
WO2016181306A1 (en) * 2015-05-12 2016-11-17 Lupin Limited Process for the preparation of efinaconazole
WO2016193917A1 (en) * 2015-06-04 2016-12-08 Glenmark Pharmaceuticals Limited Process for the preparation of efinaconazole

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
OGURA H ET AL: "Synthesis and antifungal activities of (2R,3R)-2-aryl-1-azolyl-3-(substituted amino)-2-butanol derivatives as topical antifungal agents", CHEMICAL AND PHARMACEUTICAL BULLETIN, PHARMACEUTICAL SOCIETY OF JAPAN, JP, vol. 47, no. 10, 1 October 1999 (1999-10-01), pages 1417 - 1425, XP002759239, ISSN: 0009-2363, [retrieved on 20080331], DOI: 10.1248/CPB.47.1417 *
See also references of WO2016116919A1 *

Also Published As

Publication number Publication date
EP3247399A1 (en) 2017-11-29
US20180002310A1 (en) 2018-01-04
AU2015379251A1 (en) 2017-07-27
JP2018502165A (en) 2018-01-25
CN107427585A (en) 2017-12-01
IL253479A0 (en) 2017-09-28
WO2016116919A1 (en) 2016-07-28
CA2974180A1 (en) 2016-07-28

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